Abstract
A microbiological agar diffusion method (cylinder-plate method) using Candida albicans ATCC 28516 for quantitation of ketoconazole (KCZ) was established. The bioassay method was sensitive to 0.16μg/ml of KCZ in a human blood-based chemistry control material (Moni-Trol I) and linear from 0.16μg/ml to 40μg/ml. The pharmacokinetics in rats following oral administration of KCZ, at a dose of 40mg/kg, was studied by the bioassay method. KCZ appears to be well absorbed from the gastrointestinal tract. Peak plasma concentrations after a single dose was 65.6μg/ml. KCZ was widely distributed in the body tissues, including to the skin and hair. This might be one of the reasons why KCZ exhibits remarkable in vivo activities.